Bergenin review
February 2 2017 by Ray Sahelian, M.D.

Bergenin monohydrate is an isocumeric compound that is found in several herbs. It is a C-glycoside of 4-O-methyl gallic acid. Bergenin may have potential to treat cardiac arrhythmias.

Review article
Fitoterapia. 2015. Diversity, pharmacology and synthesis of bergenin and its derivatives: Potential materials for therapeutic usages. Bergenin, a natural secondary metabolite, has been isolated from different parts of a number of plants. It is one of active ingredients in herbal and Ayurvedic formulations. It exhibits antiviral, antifungal, antitussive, antiplasmodial, antiinflammatory, antihepatotoxic, antiarrhythmic, antitumor, antiulcerogenic, antidiabetic and wound healing properties.

Benefit for heart rhythm problems
Bergenin is the antiarrhythmic principle of Fluggea virosa.
Planta Med. 2002.
Bergenin was isolated from the aerial parts of Fluggea virosa. Anti-arrhythmic effects of bergenin were investigated. It showed distinct therapeutic effects on BaCl2-induced arrhythmias in rats. At concentrations of 0.4 mg/kg and 0.8 mg/kg bergenin significantly countered arrhythmias induced by ligation and reperfusion of the coronary artery. At 0.8 mg/kg, bergenin elevated the atria fibrillation threshold in rabbits from 1.3 mV to 1.9 mV. Our results suggest that bergenin has good potential to treat cardiac arrhythmias.

Some plants that have bergenin
Ardisia colorata fruits have ardisiphenols, bergenin, a bergenin derivative demethoxybergenin, alkylresorcinols, embelin, myricetin, quercetin, norbergenin, kaempferol, quercetin-3-O-beta-D-glucopyranoside and gallic acid.
Ardisia japonica has about 50 to 60 percent bergenin. The content of bergenin in Ardisia pusilla and Ardisia japonica is similar.
Astilbe chinensis has bergenin
Astilbe thunbergii
Bergenia crassifolia
Bergenia ligulata herb has bergenin and gallic acid.
Bergenia stracheyi
Flueggea virosa leaves have a good amount of bergenin.
Mallotus japonicus has a good amount of bergenin. Norbergenin, which is the O-demethyl derivative of bergenin, the main component of Mallotus japonicus, has moderate antioxidant activity.
Mallotus roxburghianus is used in the traditional medicine in North-Eastern India and contains bergenin.
Sacoglottis gabonensis bark has bergenin.

Antioxidant properties
Antioxidant activity of bergenin: a phytoconstituent isolated from the bark of Sacoglottis uchi Huber (Humireaceae).
Org Biomol Chem. 2008; De Abreu HA, Aparecida Dos S Lago I, Souza GP, Piló-Veloso D, de C Alcântara AF. Departamento de Química,Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.
Bergenin was isolated from Sacoglottis uchi, a species of vegetable found in the Amazon region and popularly used for the treatment of several hepatic problems. This phytoconstituent has been used as an oriental folk medicine for the treatment of many diseases and shows liver protecting properties. We confirmed the antioxidant properties of bergenin.

Bergenin research studies
Protective effects of bergenin, the major constituent of Mallotus japonicus, on D-galactosamine-intoxicated rat hepatocytes.
J Ethnopharmacol. 2000.
This study was designed to investigate the effects of bergenin against D-galactosamine-induced injury in primary cultured rat hepatocytes. Bergenin decreased the release of glutamic pyruvic transaminase and sorbitol dehydrogenase into hepatocyte medium incubated for galactosamine. The present results suggest that bergenin show liver protective effects against galactosamine-intoxicated rat hepatocytes by inhibiting the release of glutamic pyruvic transaminase and sorbitol dehydrogenase as well as by increasing RNA synthesis.

Antihepatotoxic activity of bergenin, the major constituent of Mallotus japonicus, on carbon tetrachloride-intoxicated hepatocytes.
J Ethnopharmacol. 2000.
To determine the antihepatotoxic activity of bergenin from Mallotus japonicus, carbon tetrachloride (CCl4)-induced cytotoxicity in primary cultured rat hepatocytes has been adopted as an assay system. Bergenin significantly reduced the activities of glutamic pyruvic transaminase and sorbitol dehydrogenase released from the CCl4-intoxicated liver cells. The antihepatotoxicity of bergenin was also evidenced by elevating the activities of glutathione S-transferase and glutathione reductase, and content of glutathione in the CCl4-intoxicated hepatocytes. From these results, it is assumed that bergenin exerted antihepatotoxicity against CCl4-induced cytotoxicity through glutathione-mediated detoxification as well as free radical suppressing activity.

How to easily replace the independent atom model - the example of bergenin, a potential anti-HIV agent of traditional Asian medicine.
Acta Crystallogr B. 2009; Dittrich B, Weber M, Kalinowski R, Grabowsky S, Hübschle CB, Luger P. Institut für Anorganische Chemie, Georg-August-Universität Göttingen, Tammanstrasse 4, Göttingen, Germany.
Bergenin, which has been isolated from a variety of tropical plants, has several pharmacological applications in traditional Asian medicine. Its electron-density distribution was obtained from a room-temperature low-resolution X-ray data set measured with point detection making use of multipole populations from the invariom library. Two refinement models were considered. In a first step, positional parameters and ADPs were refined with fixed library multipoles (model E1). This model was suitable to be input into a second refinement of multipoles (model E2), which converged smoothly although based on Cu Kalpha room-temperature data. Quantitative results of a topological analysis of the electron density from both models were compared with Hartree-Fock and density-functional calculations. With respect to the independent atom model (IAM) more information can be extracted from invariom modelling, including the electrostatic potential and hydrogen-bond energies, which are highly useful, especially for biologically active compounds. The reliability of the applied invariom formalism was assessed by a comparison of bond-topological properties of sucrose, for which high-resolution multipole and invariom densities were available. Since a conventional X-ray diffraction experiment using basic equipment was combined with the easy-to-use invariom formalism, the procedure described here for bergenin illustrates how it can be routinely applied in pharmacological research.

Absorption of bergenin
Kinetics study on intestinal absorption of bergenin in rats.
Sichuan Da Xue Xue Bao Yi Xue Ban. 2007. Key Laboratory of Drug Targeting of Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, China.
To study the kinetics of intestine absorption of bergenin in rats. The intestine absorption of bergenin in the rats was determined by in situ perfusion. The HPLC were used to determine the concentration of bergenin in the perfusate and the plasma. The concentrations of bergenin in various sites of the intestine and the pH values were studied. The absorption of bergenin exhibited linear kinetics. The absorption varied in the duodenum, jejunum, ileum and colon. In the range of pH 5.4-7.8, with the increasing of pH value, the Ka of bergenin decreased. Bergenin is absorbed by the entire intestine, but with limited amount. The absorption of the drug is a first-order process with the passive diffusion mechanism.

Constituents of Ardisia japonica and their in vitro anti-HIV activity
J Nat Prod. 1996.
As part of our screening of anti-AIDS agents from medicinal plants, the MeOH extract of the aerial parts of Ardisia japonica was tested, and it showed moderate in vitro anti-HIV activity. Reexamination to identify the compounds responsible for the anti-HIV activity revealed several known compounds and a new triterpenoid saponin. All of the isolated compounds were tested and, although none of the triterpenoid saponins was active, bergenin and norbergenin showed weak anti-HIV activity.

Studies on the chemical constituents of Ardisia crenata Sims
Zhongguo Zhong Yao Za Zhi. 1989.
A new bergenin derivative isolated from the root of Ardisia crenata was determined to be 11-o-syringylbergenin by spectral methods. Other compounds were identified as spinasterol, series fatty acids, beta-sitosterol-beta-D-glucoside, norbergenin and sucrose respectively. The last three were obtained for the first time from the genus of Ardisia.